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BRK inhibitor P21d

Chemical Structure : BRK inhibitor P21d

CAS No.: 1338249-87-8

BRK inhibitor P21d

Catalog No.: PC-35189Not For Human Use, Lab Use Only.

BRK inhibitor P21d is a potent, selective, cell permeable inhibitor of breast tumor kinase (Brk, PTK6) with IC50 of 30 nM, shows no inhibitory activity against Aurora B and Lck (IC50>20 uM).

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

BRK inhibitor P21d is a potent, selective, cell permeable inhibitor of breast tumor kinase (Brk, PTK6) with IC50 of 30 nM, shows no inhibitory activity against Aurora B and Lck (IC50>20 uM); exhibits potent cellular activity with p-SAM68 IC50 of 52 nM, downregulates SNAIL protein and restores E-cadherin expression in TNBC cells; suppresses migration of MDA-MB-231 and MMTV-myc cells, sensitizes TNBC cells to anoikis and suppresses metastasis formation.

Physicochemical Properties

M.Wt 447.474
Formula C23H22FN7O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(4-((6-cyclopropyl-3-(1H-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-yl)amino)-3-fluorophenyl)(morpholino)methanone

References

1. Zeng H, et al. Bioorg Med Chem Lett. 2011 Oct 1;21(19):5870-5.

2. Ito K, et al. Cancer Res. 2016 Aug 1;76(15):4406-17.

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